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Powders for reconstitution

a technology of reconstitution and powder, which is applied in the direction of biocide, drug composition, dispersed delivery, etc., can solve the problems of resistance, no currently available drug therapy is capable of completely eradicating hiv, and emergence of resistant mutants

Active Publication Date: 2010-05-13
JANSSEN SCI IRELAND UC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to the use of a powder containing TMC278, dispersed in a water-soluble polymer, for the manufacture of a medicament for the treatment of HIV infection. The powder can be mixed with water to create a supersaturated solution or a suspension for injection. The invention provides a method for treating HIV infection by administering the supersaturated solution to a patient. The invention also provides a process for preparing the supersaturated solution by adding water to a powder of TMC278. The compound TMC278 is a potent inhibitor of HIV and is currently in clinical development.

Problems solved by technology

The treatment of Human Immunodeficiency Virus (HIV) infection, known as cause of the acquired immunodeficiency syndrome (AIDS), remains a major medical challenge.
Although effective in suppressing HIV, each of these drugs, when used alone, is confronted with the emergence of resistant mutants.
However, none of the currently available drug therapies is capable of completely eradicating HIV.
Even HAART can face the emergence of resistance, often due to non-adherence to and non-persistence with antiretroviral therapy.
Paediatric anti-HIV medication poses particular challenges in that the dose regimens vary to a large extent due to variations in age and body weight (babies—children).
Traditional dosage forms such as pills and capsules lack the dosing flexibility required in paediatric applications.
Moreover, these dosage forms are not fit for administration to young children and especially to infants in which case drinkable formulations are the preferred route of administration.
Incorporating TMC278 in a powder for reconstitution poses particular challenges in that it is poorly soluble in water.
Upon addition of water, only a limited amount is dissolved not resulting in effective uptake of the active ingredient.
For paediatric applications these salts are unattractive because of their low pH.

Method used

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  • Powders for reconstitution

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0069]4 g TMC278 base and 36 g PVP-VA 64 are dissolved in 800 ml of a mixture of methanol / methylene chloride 50:50 (v / v). This mixture is spray dried at 80° C. (inlet temperature) using a Mini Spray Dryer B-191 (Büchi, Switzerland). The flow control was set at 800 N 1 / h pressurized air, the aspirator at 100% and the pump at 50%. Afterwards, the resulting powders were post dried in a vacuum dryer (Christ Alpha, Medizinischer Apparatebau, OsterodelHarz, Germany) for 44 hours.

example 2

[0070]4 g TMC278 base, 34 g PVP-VA 64 and 2 g Cremophor EL are dissolved in 800 ml of a mixture of methanol / methylene chloride 50:50 (v / v). This mixture is the spray dried at 80° C. (inlet temperature) using a Mini Spray Dryer B-191 (Büchi, Switzerland). The flow control was set at 800 N 1 / h pressurized air, the aspirator at 100% and the pump at 50%. Afterwards, the resulting powders were post dried in a vacuum dryer (Christ Alpha, as above) for 44 hours.

[0071]Dissolution:

[0072]The powders for reconstitution of example 1 and 2 were tested on dissolution. During the dissolution test, the powders for reconstitution of TMC278 was suspended into 50 ml of water and the resulting suspension was added into 500 ml of the 0.01 M HCl aqueous solution serving as dissolution medium resulting in a final suspension volume of 550 ml. At each time point, 5.0 ml of the final suspension was removed and the volume was compensated by adding 5.0 ml of fresh dissolution medium. So, to calculate the % of ...

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Abstract

This invention relates to powders for reconstitution comprising the NNRTI TMC278 dispersed in certain water-soluble polymers, which can be used in the treatment of HIV infection.

Description

FIELD OF THE INVENTION [0001]This invention relates to powders for reconstitution comprising the NNRTI TMC278 dispersed in certain water-soluble polymers, useful in the treatment of HIV infection.BACKGROUND OF THE INVENTION[0002]The treatment of Human Immunodeficiency Virus (HIV) infection, known as cause of the acquired immunodeficiency syndrome (AIDS), remains a major medical challenge. HIV is able to evade immunological pressure, to adapt to a variety of cell types and growth conditions, and to develop resistance against currently available drug therapies. The latter include nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), HIV-protease inhibitors (PIs), and the more recent fusion inhibitors.[0003]Although effective in suppressing HIV, each of these drugs, when used alone, is confronted with the emergence of resistant mutants. This led to the introduction of combinat...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/505A61P31/18
CPCA61K9/0095Y10S514/934A61K9/1635A61K9/08A61P31/18A61K9/14A61K47/34A61K47/38
Inventor BAERT, LIEVEN ELVIRE COLETTEVAN GYSEGHEM, ELKEVAN DEN MOOTER, GUY RENE JAAKVAN REMOORTERE, PETER JOZEF MARIA
Owner JANSSEN SCI IRELAND UC